Biological Information

Background Information:

Adrenoreceptors belong to the superfamily of G protein-coupled seven transmembrane proteins. G-protein-coupled receptors constitute one of the major signal transduction systems in eukaryotic cells. Coding sequences for these receptors, in those regions believed to contribute to the agonist-antagonist binding site, are strongly conserved across mammalian species. Adrenoreceptors are found in most peripheral tissue and within the central nervous system.

Family:

GPCR

Sub Family:

Adrenoceptor

Class:

Class A

Protein Name:

alpha1D

Uniprot Number:

P25100

Protein Aliases:

Alpha-1D adrenoreceptor|Alpha-1D adrenoceptor|Alpha-adrenergic receptor 1a

Gene Name:

ADRA1D

Gene ID:

146

Gene Aliases:

ADRA1R|ADRA1A|ADRA1

Accession Number:

NM_000678

Organism:

Human

Construct Details:

Full Length, Recombinant

Cell Type:

HEK293

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

Detection Method:

TR-FRET

Measured Response:

Fluorescence

Testing Information

Incubation:

1 hr at 37°C

Control Inhibitor:

Bmy-7378

Criteria For Significance:

≥ 50% increase in IP-one relative to Phenylephrine response, ≥ 50% Inhibition of Phenylephrine-induced response

Test Concentration / Dose:

Compounds are screened at 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.003 μM

Test Sample Requirements:

75 μl of 10 mM stock or 1 mg (pre-weighed) powder (assuming FW ≦500 and purity 100%)

Minimum Order Quantity:

16

Turnaround Time

Standard:

20 Business Days

Reference Compound Data

PubChem ID

2419

Name

Bmy-7378

Measurement

0.0034μM - IC50

PubChem ID

4893

Name

Prazosin

Measurement

0.0005μM - IC50

PubChem ID

92766

Name

Corynanthine

Measurement

0.16μM - IC50

Clinical Relevance

Therapeutic Area:

Cardiovascular

Adverse / Beneficial Action:

Adrenergic a1D receptor antagonism may be useful in the treatment of hypertension with minimal associated orthostatic hypotension.

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

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